G007-LK
- CAS No.
- 1380672-07-0
- Chemical Name:
- G007-LK
- Synonyms
- G007-LK;CS-1659;G007 LK;G007LK;G007-LK;G007 LK;G007LK;Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem;G007LK,Inhibitor,poly ADP ribose polymerase,G-007-LK,G007 LK,PARP,inhibit,G007-LK;(E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile;4-[5-[(1E)-2-[4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile;Benzonitrile, 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-
- CBNumber:
- CB32707548
- Molecular Formula:
- C25H16ClN7O3S
- Molecular Weight:
- 529.96
- MDL Number:
- MFCD28167833
- MOL File:
- 1380672-07-0.mol
- MSDS File:
- SDS
G007-LK price More Price(22)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 5.04907 | Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem Tankyrase 1/2 Inhibitor VI, G007-LK, CAS 1380672-07-0, is a cell-permeable, potent and highly selective inhibitor of tankyrase (IC50 = 33 & 26 nM for TNKS1 and TNKS2, respectively). | 1380672-07-0 | 10MG | $280 | 2024-03-01 | Buy |
| Cayman Chemical | 22934 | G007-LK ≥98% | 1380672-07-0 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 22934 | G007-LK ≥98% | 1380672-07-0 | 5mg | $139 | 2024-03-01 | Buy |
| Cayman Chemical | 22934 | G007-LK ≥98% | 1380672-07-0 | 10mg | $243 | 2024-03-01 | Buy |
| Cayman Chemical | 22934 | G007-LK ≥98% | 1380672-07-0 | 25mg | $533 | 2024-03-01 | Buy |
G007-LK Chemical Properties,Uses,Production
General Description
A cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD+ pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC50 = 33 and 26 nM, respectively, against TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 in auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (ICmax ~300 and 600 nM, respectively). Shown to display little or no inhibitory potency (IC50 >10 μM) toward 7 other PARP enzymes (PARP1, 2, 3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC50 >10 μM). Shown to inhibit two CRC lines, COLO-320DM & SW403, colony formation in vitro (200 nM) and tumor expansion in mice in vivo (20 mg/kg via daily i.p.), although G007-LK toxicity is observed at higher dosages (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biological Activity
g007-lk is a potent and specific inhibitor of tankyrase 1/2 with ic50 values of 46 and 25 nm [1].the telomeric repeat factor 1 (trf1)-interacting ankyrin-related adp-ribose polymerase 1 (tankyrase 1,tnks1) and tankyrase 2 (tnks2) belong to the subgroup of poly(adp-ribosyl)ating polymerases and regulate the assembly and disassembly of large polymerized structures [1].g007-lk is a potent and specific tankyrase 1/2 inhibitor. g007-lk reduced auto-poly-(adp ribosy)lation of tnks1 and tnks2 with ic50 values of 46 nm and 25 nm, respectively. in wnt3a-induced hek 293 cells, g007-lk inhibited st-luc with ic50 value of 0.05 μm [1]. in sw480 colorectal cancer cell line transfected with gfp-tnks1, g007-lk induces highly dynamic and mobile degradasomes containing phosphorylated beta-catenin, beta-trcp and ubiquitin [2]. in the apc-mutant cell lines, g007-lk reduces cytosolic and nuclear β-catenin protein levels [3].in mice bearing colo-320dm cell xenografts, g007-lk (20 mg/kg twice daily or 40 mg/kg daily) concentration-dependently inhibited tumor growth by 61% and 48%, respectively. also, g007-lk reduced the levels of tnks1/2 and β-catenin, and stabilized axin1/2 [3].
Biochem/physiol Actions
Cell permeable: yes
References
[1]. voronkov a, holsworth dd, waaler j, et al. structural basis and sar for g007-lk, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor. j med chem, 2013, 56(7): 3012-3023.
[2]. thorvaldsen te, pedersen nm, wenzel em, et al. structure, dynamics and functionality of tankyrase inhibitor-induced degradasomes. mol cancer res, 2015, pii: molcanres.0125.2015.
[3]. lau t, chan e, callow m, et al. a novel tankyrase small-molecule inhibitor suppresses apc mutation-driven colorectal tumor growth. cancer res, 2013, 73(10): 3132-3144.
G007-LK Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
View Lastest Price from G007-LK manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
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2020-01-02 | (E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile
1380672-07-0
|
US $1.00 / KG | 1KG | Min98% HPLC | g/kg/ton | Career Henan Chemical Co |
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- (E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile
1380672-07-0
- US $1.00 / KG
- Min98% HPLC
- Career Henan Chemical Co